General
Preferred name
METHOCARBAMOL
Synonyms
Metocarbamol ()
Lumirelax ()
AHR 85 ()
Robaxin ()
Miolaxin ()
Robaxin-750 ()
Forbaxin ()
Methocarbamol component of robaxisal ()
NSC-170960 ()
Delaxin ()
Neuraxin ()
Methocarbamol-d5 ()
P&D ID
PD001863
CAS
532-03-6
3967-43-9
145308-03-8
1189699-70-4
Tags
available
drug
Approved by
FDA
First approval
1957
Drug Status
vet_approved
approved
Max Phase
4.0
Drug indication
cirrhosis of liver
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
METABOLISM Methocarbamol is metabolized in the liver by demethylation to 3-(2-hydroxyphenoxy)-1,2-propanediol-1-carbamate or hydroxylation to 3-(4-hydroxy-2-methoxyphenoxy)-1,2-propanediol-1-carbamate.[A178366] Methocarbamol and its metabolites are conjugated through glucuronidation or sulfation.[A178366]
PHARMACODYNAMICS Methacarbamol is a skeletal muscle relaxant with an unknown mechanism of action.[A178426] Methacarbamol has been shown to block spinal polysynaptic reflexes, decrease nerve transmission in spinal and supraspinal polysynaptic pathways, and prolong the refractory period of muscle cells.[A178426,A178411] Methocarbamol does not act as a local anesthetic upon injection.[A178411] In animal studies, methocarbamol also prevents convulsions after electric shock.[A178426]
MOA The mechanism of action of methocarbamol is thought to be dependant on its central nervous system depressant activity.[A31312] This action may be mediated through blocking spinal polysynaptic reflexes, decreasing nerve transmission in spinal and supraspinal polysynaptic pathways, and prolonging the refractory period of muscle cells.[A178426,A178411] Methocarbamol has been found to have no effect on contraction of muscle fibres, motor end plates, or nerve fibres.[L6268]
INDICATION Methocarbamol tablets and intramuscular injections are indicated in the United States as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions.[Label,L6268] Oral methocarbamol in America may be given up to 1500mg 4 times daily for 2-3 days.[A31312]; ; In Canada, methocarbamol containing oral formulations are sold over the counter for pain associated with muscle spasm.[L6295] However, if these combination formulations include codeine, they are prescription only.[L6295]
ROE In humans the majority of the dose is eliminated in the urine.[A178366] In dogs, 88.85% of the dose is eliminated in urine and 2.14% in the feces.[A178366] In rats, 84.5-92.5% of the dose is eliminated in the urine and 0-13.3% is eliminated in the feces.[A178366]
TOXICITY Overdose of methocarbamol may be associated with alcohol and other central nervous system depressants.[Label] Patients may experience nausea, drowsiness, blurred vision, hypotension, seizures, and coma.[Label] Treatment of overdose is generally through airway maintenance, monitoring urinary output, vital signs, and giving fluid intravenously if necessary.[Label]; ; The oral LD50 in rats is 3576.2mg/kg.[L6295]; ; The FDA has classified methocarbamol as pregnancy category C.[Label] Animal and human studies have not been performed to determine the risks to a fetus, however fetal and congenital abnormalities have been reported.[Label] Methocarbamol is excreted in the milk of dogs, however it is unknown if this is also the case for humans.[Label] Caution should be exercised when taking methocarbamol while breastfeeding.[Label]; ; Studies to assess the carcinogenicity, mutagenicity, or effects on fertility of methocarbamol have not been performed.[Label]
HALF-LIFE The elimination half life is 1.14 hours in healthy subjects and 1.24 hours in subjects with renal insufficiency.[A636] Older studies report half lives of 1.6-2.15 hours.[A178366]
ABSORPTION The time to maximum concentration is 1.1 hours for both healthy patients and those on hemodialysis.[A636] The maximum plasma concentration is 21.3mg/L for healthy patients and 28.7mg/L in hemodialysis patients.[A636] The area under the curve for healthy patients is 52.5mg/L\*hr and 87.1mg/L*hr in hemodialysis patients.[A636] AUC% based on terminal elimination half life is 2% for healthy patients and 4% for hemodialysis patients.[A636]; ; Older studies report maximum plasma concentrations in 0.5 hours.[A178366]
DESCRIPTION Methocarbamol is the carbamate of , but the carbamate bond is not metabolically hydrolysed, so guaifenesin is not a metabolite of methocarbamol. Methocarbamol has reduced abuse potential compared to other carbamate drugs such as and its prodrug . (GtoPdb)
DESCRIPTION Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research[1][2][3].
PRICE 29
DESCRIPTION Methocarbamol is a CNS depressant. It is an orally bioavailable skeletal muscle relaxant. Methacarbamol has been shown to block spinal polysynaptic reflexes, decrease nerve transmission in spinal and supraspinal polysynaptic pathways, and prolong the refractory period of muscle cells. (Enamine Bioactive Compounds)
DESCRIPTION Methocarbamol (AHR 85) is a centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (TargetMol Bioactive Compound Library)
Compound Sets
22
Cayman Chemical Bioactives
23870
33464
ChEMBL Approved Drugs
CHEMBL1201117
ChEMBL Drugs
CHEMBL1201117
CZ-OPENSCREEN Bioactive Library
DrugBank
DB00423
DrugBank Approved Drugs
DB00423
DrugCentral
1747
DrugCentral Approved Drugs
1747
DrugMatrix
Enamine Bioactive Compounds
EBC-03743
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101177
Guide to Pharmacology
6829
MedChem Express Bioactive Compound Library
HY-B0262
NCATS Inxight Approved Drugs
125OD7737X
NIH Clinical Collections (NCC)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
Methocarbamol(Robaxin)
TargetMol Bioactive Compound Library
T1409
The Spectrum Collection
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
241.1
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
1
Aromatic Ring Count
1
cLogP
0.53
TPSA
91.01
Fraction CSP3
0.36
Chiral centers
1.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
CA1
Sodium Channel
Carbonic Anhydrase
Pathway
Membrane Transporter/Ion Channel
Metabolism
Source data